Polyaphron Dispersion Topical Composition for Atopic Dermatitis
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Solution Overview
Problem
Current crisaborole formulations for atopic dermatitis have poor aesthetic profiles, limited patient compliance, and instability issues, particularly in cream forms, which can affect skin permeation and stability.
Innovation Solution
A topical composition using a polyaphron dispersion with a continuous aqueous phase and a discontinuous oil phase, incorporating crisaborole, which maintains high solubility and stability, improving both aesthetic profile and skin penetration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a non-aqueous ointment formulation is used, then skin permeation and chemical stability are improved, but aesthetic profile and patient compliance deteriorate
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by introducing a polyaphron dispersion system with specific HLB value surfactants, transforming the traditional non-aqueous ointment into a water-containing cream that maintains permeation efficacy while improving aesthetics
Solution Approach 2:
The patent creates a composite formulation system combining aqueous and non-aqueous phases within a polyaphron dispersion structure, where the continuous aqueous phase provides aesthetic benefits and the dispersed oil phase maintains drug solubility and permeation properties
2Ease of operation
If a cream formulation is used, then aesthetic profile and patient compliance are improved, but solubility and physical stability deteriorate
Solution Approach 1:
The patent optimizes the HLB value parameter of surfactants to precisely control the solubility of crisaborole in the aqueous phase, enabling high drug loading (2-10%) while maintaining physical stability and preventing crystallization
Solution Approach 2:
The patent introduces surfactants as intermediary substances that mediate between the aqueous continuous phase and crisaborole, enabling solubilization of the hydrophobic drug in the water-based cream formulation
3Ease of operation
If water is added to improve aesthetic profile, then patient compliance is improved, but chemical stability deteriorates due to hydrolysis
Solution Approach 1:
The patent controls the pH parameter of the aqueous phase and selects surfactants with appropriate HLB values to create a chemical environment that minimizes hydrolysis of crisaborole while maintaining the water-based cream formulation for aesthetic benefits
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition enhances patient compliance and skin permeation, maintaining crisaborole solubility and stability, even at high concentrations, thereby improving treatment efficacy for atopic dermatitis.
Implementation Method 1
the crisaborole is in solution in the composition
Implementation Method 2
improving both aesthetic profile and skin penetration
Data Source
AI summary
The present invention relates to a composition for topical application comprising a polyaphron dispersion, wherein the polyaphron dispersion comprises a continuous phase, a discontinuous phase and crisaborole.